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Literature summary for 1.2.1.104 extracted from

  • Liu, Y.J.; Fan, X.Y.; Zhang, D.D.; Xia, Y.Z.; Hu, Y.J.; Jiang, F.L.; Zhou, F.L.; Liu, Y.
    Dual inhibition of pyruvate dehydrogenase complex and respiratory chain complex induces apoptosis by a mitochondria-targeted fluorescent organic arsenical in vitro and in vivo (2020), ChemMedChem, 15, 552-558 .
    View publication on PubMed

Application

Application Comment Organism
medicine the acute promyelocytic leukemia is greatly alleviated in the PDT-PAO-F16 treated group in an acute promyelocytic leukemia mice model Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-[3-[4-(1,3,2-dithiarsinan-2-yl)anilino]-3-oxopropyl]-4-[(E)-2-(1H-indol-3-yl)ethenyl]pyridin-1-ium i.e. PDT-PAO-16, organic arsenal inhibitor, mainly accumulates in mitochondria within hours and suppresses the activity of the pyruvate dehydrogenase complex resulting in the inhibition of ATP synthesis and thermogenesis disorder. The suppression of respiratory chain complex I and IV accelerates the mitochondrial dysfunction leading to caspase family-dependent apoptosis. In vivo, the acute promyelocytic leukemia is greatly alleviated in the PDT-PAO-F16 treated group in an acute promyelocytic leukemia mice model Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P08559 and P11177 and O00330 and P10515 and P09622 P08559 i.e. subunit PdhA1, cf. EC 1.2.4.1, P11177 i.e. subunit PdhB1, cf. EC 1.2.4.1, O00330 i.e. subunit PdhX, P10515 i.e. subunit DlaT, cf. EC 2.3.1.12, P09622 i.e. subunit Dld, cf. EC 1.8.1.4, respectively
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Source Tissue

Source Tissue Comment Organism Textmining
NB-4 cell
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Homo sapiens
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